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HRID 38075作成日:2026年10月26日

4-Methylmorpholine → 3-fluoro-N-[3-(7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-benzenesulfonamide

https://huagongshe.com/reaction/38075

反応式

関与物質

役割名称HCID仕込み量
反応物4-MethylmorpholineHCID 7972—
反応物3-Fluorobenzenesulfonyl ChlorideHCID 2734258—
反応物3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenylamineHCID 46929183—
溶媒DichloromethaneHCID 6344—
生成物3-fluoro-N-[3-(7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-benzenesulfonamideHCID 5847709058.5%

反応手順

3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenylamine (prepared as described in Example 1) (30 mg, 0.102 mmol) was dissolved in dry DCM (1 mL). At room temperature 3-fluorobenzensulfonylchloride (0.014 mL, 0.107 mmol, 1.05 eq) was added followed by NMM (0.012 mL, 0.107 mmol, 1.05 eq) and the mixture was stirred for 1 hour. It was then diluted with DCM and washed with water and brine. The organic layer was dried over Na2SO4 and concentrated under reduced pressure. The crude product was purified by chromatography on silica gel (eluant DCM/MeOH 96:4) to give 27 mg of 3-fluoro-N-[3-(7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-benzenesulfonamide.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08524707B2
出典データセットuspto-grants-2013_09
ORD IDord-66e88c0f0e00469c854c41e01f9ef212
出典メモuspto-grants-2013_09